TWI814234B - 突變蛋白抑制劑的製備及其應用 - Google Patents

突變蛋白抑制劑的製備及其應用 Download PDF

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Publication number
TWI814234B
TWI814234B TW111103959A TW111103959A TWI814234B TW I814234 B TWI814234 B TW I814234B TW 111103959 A TW111103959 A TW 111103959A TW 111103959 A TW111103959 A TW 111103959A TW I814234 B TWI814234 B TW I814234B
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Taiwan
Prior art keywords
compound
base
esi
methoxy
fluoro
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TW111103959A
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English (en)
Chinese (zh)
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TW202237604A (zh
Inventor
梁永宏
許志勇
曾兆森
嚴文廣
熊方均
Original Assignee
大陸商藥雅科技(上海)有限公司
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Priority claimed from CN202110276073.3A external-priority patent/CN115073450A/zh
Priority claimed from CN202110374457.9A external-priority patent/CN115160309B/zh
Priority claimed from CN202110496041.4A external-priority patent/CN115304603B/zh
Priority claimed from CN202110672205.4A external-priority patent/CN115490689B/zh
Application filed by 大陸商藥雅科技(上海)有限公司 filed Critical 大陸商藥雅科技(上海)有限公司
Publication of TW202237604A publication Critical patent/TW202237604A/zh
Application granted granted Critical
Publication of TWI814234B publication Critical patent/TWI814234B/zh

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
TW111103959A 2021-03-15 2022-01-28 突變蛋白抑制劑的製備及其應用 TWI814234B (zh)

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
CN202110276073.3 2021-03-15
CN202110276073.3A CN115073450A (zh) 2021-03-15 2021-03-15 Krasg12c突变蛋白抑制剂的制备及其应用
CN202110374457.9 2021-04-07
CN202110374457.9A CN115160309B (zh) 2021-04-07 2021-04-07 Krasg12c突变蛋白杂环类抑制剂的制备及其应用
CN202110496041.4 2021-05-07
CN202110496041.4A CN115304603B (zh) 2021-05-07 2021-05-07 喹唑啉类抑制剂的制备及其应用
CN202110672205.4 2021-06-17
CN202110672205.4A CN115490689B (zh) 2021-06-17 2021-06-17 不可逆krasg12c抑制剂的制备及其应用

Publications (2)

Publication Number Publication Date
TW202237604A TW202237604A (zh) 2022-10-01
TWI814234B true TWI814234B (zh) 2023-09-01

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Family Applications (1)

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TW111103959A TWI814234B (zh) 2021-03-15 2022-01-28 突變蛋白抑制劑的製備及其應用

Country Status (3)

Country Link
US (1) US20240182470A1 (fr)
TW (1) TWI814234B (fr)
WO (1) WO2022193982A1 (fr)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20230107642A1 (en) 2020-12-18 2023-04-06 Erasca, Inc. Tricyclic pyridones and pyrimidones
WO2023114733A1 (fr) * 2021-12-13 2023-06-22 Quanta Therapeutics, Inc. Modulateurs de kras et leurs utilisations
WO2023154766A1 (fr) 2022-02-09 2023-08-17 Quanta Therapeutics, Inc. Modulateurs de kras et leurs utilisations
CN118660891A (zh) * 2022-02-14 2024-09-17 深圳福沃药业有限公司 作为kras g12c突变抑制剂的喹唑啉衍生物

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016164675A1 (fr) * 2015-04-10 2016-10-13 Araxes Pharma Llc Composés quinazoline substitués et leurs procédés d'utilisation
WO2020239077A1 (fr) * 2019-05-29 2020-12-03 上海翰森生物医药科技有限公司 Régulateur dérivé hétérocyclique contenant de l'azote, son procédé de préparation et son application
CN112110918A (zh) * 2019-06-21 2020-12-22 劲方医药科技(上海)有限公司 螺环取代的嘧啶并环类化合物,其制法与医药上的用途
CN112142735A (zh) * 2020-04-09 2020-12-29 上海凌达生物医药有限公司 一类稠和氰基吡啶类化合物、制备方法和用途
WO2021031952A1 (fr) * 2019-08-16 2021-02-25 劲方医药科技(上海)有限公司 Composé de pyrimidine cyclique à six chaînons substitué par oxygène, son procédé de préparation et son utilisation médicale

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021139678A1 (fr) * 2020-01-07 2021-07-15 广州百霆医药科技有限公司 Inhibiteur pyridopyrimidine de protéine mutante kras g12c
WO2021168193A1 (fr) * 2020-02-20 2021-08-26 Beta Pharma, Inc. Dérivés de pyridopyrimidine en tant qu'inhibiteurs de kras
KR20230019101A (ko) * 2020-04-29 2023-02-07 상하이 린진 바이오파마 씨오., 엘티디. 벤조티아졸릴 비아릴 화합물, 제조 방법 및 용도
CN113754653A (zh) * 2020-06-05 2021-12-07 明慧医药(上海)有限公司 一种kras g12c抑制剂化合物及其用途
US20230081426A1 (en) * 2020-09-18 2023-03-16 Plexxikon Inc. Compounds and methods for kras modulation and indications therefor

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016164675A1 (fr) * 2015-04-10 2016-10-13 Araxes Pharma Llc Composés quinazoline substitués et leurs procédés d'utilisation
WO2020239077A1 (fr) * 2019-05-29 2020-12-03 上海翰森生物医药科技有限公司 Régulateur dérivé hétérocyclique contenant de l'azote, son procédé de préparation et son application
CN112110918A (zh) * 2019-06-21 2020-12-22 劲方医药科技(上海)有限公司 螺环取代的嘧啶并环类化合物,其制法与医药上的用途
WO2021031952A1 (fr) * 2019-08-16 2021-02-25 劲方医药科技(上海)有限公司 Composé de pyrimidine cyclique à six chaînons substitué par oxygène, son procédé de préparation et son utilisation médicale
CN112142735A (zh) * 2020-04-09 2020-12-29 上海凌达生物医药有限公司 一类稠和氰基吡啶类化合物、制备方法和用途

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US20240182470A1 (en) 2024-06-06
WO2022193982A1 (fr) 2022-09-22
TW202237604A (zh) 2022-10-01

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